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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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R414051-1mg | 1mg | In stock | $30.90 | |
R414051-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $127.90 | |
R414051-10mg | 10mg | In stock | $206.90 | |
R414051-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $465.90 | |
R414051-50mg | 50mg | In stock | $682.90 | |
R414051-100mg | 100mg | In stock | $1,157.90 | |
R414051-250mg | 250mg | In stock | $2,605.90 |
FGFR Inhibitors
Synonyms | Roblitinib|FGF401|1708971-55-4|FGF-401|Roblitinib [INN]|N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide|M64JF6WMSA|NVP-FGF401|N-(5-cyano-4-((2-methoxyethyl)am |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.FGF-401 is a FGF |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of fibroblast growth factor receptor 4 |
Product Description | FGF401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, FGF401 binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival. Information Roblitinib (FGF401) Roblitinib (FGF401) is an FGFR4 -selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays. Targets FGFR4 (Cell-free assay) 1.1 nM In vitro Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and it inhibits FGFR4 with an IC50 of 1.1 nM. In biochemical assays, it shows at least 1,000 fold selectivity against of panel of 65 kinases and in a kinome wide scan, consisting of 456 kinases, FGFR4 was the only target of NVP-FGF401. FGF401 inhibits growth of HCC and gastric cancer cell lines expressing FG19, FGFR4 and βklotho. In vivo In xenograft animal models NVP-FGF401 showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumor robustly inhibited in a dose dependent manner. It has good oral PK properties and remarkable anti-tumor activity in mice bearing HCC tumor xenografts and PDX models that are positive for FGF19, FGFR4 and KLB. |
ALogP | 0.939 |
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HBD Count | 2 |
Rotatable Bond | 8 |
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IUPAC Name | N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide |
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INCHI | InChI=1S/C25H30N8O4/c1-31-7-8-32(23(35)15-31)14-18-10-17-4-3-6-33(24(17)29-21(18)16-34)25(36)30-22-11-20(27-5-9-37-2)19(12-26)13-28-22/h10-11,13,16H,3-9,14-15H2,1-2H3,(H2,27,28,30,36) |
InChi Key | BHKDKKZMPODMIQ-UHFFFAOYSA-N |
Canonical SMILES | CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O |
Isomeric SMILES | CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O |
PubChem CID | 118036971 |
Molecular Weight | 506.56 |
PubChem CID | 118036971 |
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BindingDB Ligand | 209325 |
CAS Registry No. | 1708971-55-4 |
RCSB PDB Ligand | FGF |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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K2210036 | Certificate of Analysis | Jul 11, 2022 | R414051 |
K2210056 | Certificate of Analysis | Jul 11, 2022 | R414051 |
K2210057 | Certificate of Analysis | Jul 11, 2022 | R414051 |
K2210058 | Certificate of Analysis | Jul 11, 2022 | R414051 |
K2210119 | Certificate of Analysis | Jul 11, 2022 | R414051 |
Solubility | Solubility (25°C) In vitro DMSO: 6 mg/mL (11.84 mM); Water: Insoluble; Ethanol: Insoluble; |
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DMSO(mg / mL) Max Solubility | 5 |
DMSO(mM) Max Solubility | 9.87049905243209 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Weiss A, Adler F, Buhles A, Stamm C, Fairhurst RA, Kiffe M, Sterker D, Centeleghe M, Wartmann M, Kinyamu-Akunda J et al.. (2019) FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.. Mol Cancer Ther, 18 (12): (2194-2206). [PMID:31409633] |